32177-89-2Relevant articles and documents
Discovery of N-{(1S,2S)-2-(3-cyanophenyl)-3-[4-(2-[18F] fluoroethoxy)phenyl]-1-methylpropyl}-2-methyl-2-[(5-methylpyridin-2-yl)oxy] propanamide, a cannabinoid-1 receptor positron emission tomography tracer suitable for clinical use
Liu, Ping,Lin, Linus S.,Hamill, Terence G.,Jewell, James P.,Lanza Jr., Thomas J.,Gibson, Raymond E.,Krause, Stephen M.,Ryan, Christine,Eng, Waisi,Sanabria, Sandra,Tong, Xinchun,Wang, Junying,Levorse, Dorothy A.,Owens, Karen A.,Fong, Tung M.,Shen, Chun-Pyn,Lao, Julie,Kumar, Sanjeev,Yin, Wenji,Payack, Joseph F.,Springfield, Shawn A.,Hargreaves, Richard,Burns, H. Donald,Goulet, Mark T.,Hagmann, William K.
, p. 3427 - 3430 (2008/02/10)
The discovery of a structurally distinct cannabinoid-1 receptor (CB1R) positron emission tomography tracer is described. Starting from an acyclic amide CB1R inverse agonist (1) as the lead compound, an efficient route to introduce 18F to the mo
Discovery of N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1- methylpropyl]-2-methyl-2-{[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide (MK-0364), a novel, acyclic cannabinoid-1 receptor inverse agonist for the treatment of obesity
Lin, Linus S.,Lanza Jr., Thomas J.,Jewell, James P.,Liu, Fing,Shah, Shrenik K.,Qi, Hongbo,Tong, Xinchun,Wang, Junying,Xu, Suoyu S.,Fong, Tung M.,Shen, Chun-Pyn,Lao, Julie,Xiao, Jing Chen,Shearman, Lauren P.,Stribling, D. Sloan,Rosko, Kimberly,Strack, Alison,Marsh, Donald J.,Feng, Yue,Kumar, Sanjeev,Samuel, Koppara,Yin, Wenji,Van Der Ploeg, Lex H. T.,Goulet, Mark T.,Hagmann, William K.
, p. 7584 - 7587 (2007/10/03)
The discovery of novel acyclic amide cannabinoid-1 receptor inverse agonists is described. They are potent, selective, orally bioavailable, and active in rodent models of food intake and body weight reduction. A major focus of the optimization process was to increase in vivo efficacy and to reduce the potential for formation of reactive metabolites. These efforts led to the identification of compound 48 for development as a clinical candidate for the treatment of obesity.
RADIOLABELED CANNABINOID-1 RECEPTOR MODULATORS
-
Page/Page column 38, (2010/02/10)
The present invention relates to particular radiolabeled Cannabinoid-1 (CB1) receptor modulators, and methods of using these modulators for labeling and diagnostic imaging of Cannabinoid-1 receptors in mammals, particularly humans. In addition, intermediates useful for the synthesis of the radiolabeled Cannabinoid-1 receptor modulators are also disclosed, as well as the processes for synthesizing the radiolabeled Cannabinoid-1 receptor modulators. Still further, formulations of the radiolabeled Cannabinoid-1 receptor compounds are described.
